Zomepirac

Zomepirac (McN-2783-21-98 free acid) is an orally active prostaglandin synthetase inhibitor. Zomepirac blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac can be used for the research of postoperative pain and osteoarthritis^[1][2][3][4]. In Vitro:Zomepirac potently inhibits prostaglandin synthesis in homogenised bovine seminal vesicles^[3].
Zomepirac potently inhibits Collagen (HY-NP003)-induced aggregation of human platelets in vitro^[3].
Zomepirac (0.1-10 μg/mL) is 98.5% bound to human plasma albumin in vitro^[3]. In Vivo:Zomepirac (p.o.) exhibits potent non-narcotic analgesic activity in the Acetylcholine-induced writhing test in mice, with an oral ED₅₀ of 0.84 mg/kg, and lacks narcotic-like activity in mouse tail pinch and hot plate tests^[3].
Zomepirac (5 mg/kg; p.o.; 3 times daily; 3 days) shows no physical dependence liability in the mouse Naloxone (HY-17417A) challenge jumping test^[3].
Zomepirac (p.o.) exhibits potent acute anti-inflammatory activity in the Carrageenan (HY-125474)-induced paw oedema test in rats, with an oral ED₅₀ of 0.15 mg/kg^[3].
Zomepirac (p.o.) exhibits anti-inflammatory activity in the acute adjuvant-induced arthritis test in rats, with an oral ED₅₀ of 3.9 mg/kg^[3].
Zomepirac (p.o.) exhibits analgesic activity in the chronic adjuvant-induced arthritis test in rats, with an oral ED₅₀ of 16.6 mg/kg^[3].
Zomepirac (p.o.) has ulcerogenic activity in Rattus norvegicus rats, with an oral median ulcerogenic dose (UD₅₀) of 13.9 mg/kg^[3].
Zomepirac (0.3-3 mg/kg; i.v.) reduces cerebrospinal fluid prostaglandin E₂ concentrations by ~96% in conscious cats, with effects lasting up to 5 days^[3].
Zomepirac (2-6 mg/kg; i.v.) substantially reduces spinothalamic tract cell responses to nociceptive stimuli in anaesthetised rhesus monkeys^[3].
Zomepirac (20 mg/kg; i.v.) has minimal impact on renal haemodynamics and function in anaesthetised rhesus monkeys^[3].
Zomepirac (10-40 mg/kg; p.o.; daily; 12 months) causes interstitial nephritis in monkeys^[3].
Zomepirac (p.o.; daily; 24 months) increases the incidence of adrenal tumours and hyperplasia in rats^[3].
Zomepirac (p.o.; daily; 18 months) does not cause carcinogenicity in mice^[3].